Description General description A cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays. Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: yes Primary Target Bcr-abl-expressing cells in Ba/F3.p210 Product does not compete with ATP. Reversible: yes Target IC50: 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively Packaging Packaged under inert gas Warning Toxicity: Irritant (B) Reconstitution Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Zhang, J., et al. 2010. Nature463, 501. Choi, Y., et al. 2009. J. Biol. Chem.284, 29005. Adrian, F.J., et al. 2006. Nat. Chem. Biol.2, 95.